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Milademetan (DS-3032) MDM2 Inhibitor

Name: Milademetan (DS-3032)
Brand: Selleck Chemicals
SKU: S8703
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8703

Milademetan(RAIN-32, DS-3032) is an oral, selective inhibitor of the MDM2-p53 complex that reactivates p53 to induce cancer cell apoptosis and exhibits an anti-tumor effect.

Milademetan (DS-3032) MDM2/MDMX inhibitor Chemical Structure

Quality Control

Batch: S870301 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 99.63%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.63

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other MDM2/MDMX Inhibitors	Nutlin-3 RG-7112 Nutlin-3a Brigimadlin Idasanutlin (RG7388) SAR405838 NSC 207895 NVP-CGM097 Siremadlin (HDM201) Nutlin-3b

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (161.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (0.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	618.53	Formula	C₃₀H₃₄Cl₂FN₅O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1398568-47-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC₅₀/Ki	MDM2-p53
References	[1] https://pubmed.ncbi.nlm.nih.gov/36669146/ [2] https://aacrjournals.org/mct/article/22/12_Supplement/B034/730753/Abstract-B034-A-phase-2-basket-study-of-the-oral

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2023-12-21)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05932667	TERMINATED	Advanced or Metastatic Breast Cancer	Institut Curie	2023-10-12	PHASE2
NCT05012397	TERMINATED	Solid Tumors; Head and Neck Carcinoma; Cholangiocarcinoma; Sarcoma; Lung Adenocarcinoma; Bladder Urothelial Carcinoma; Stomach Adenocarcinoma; Breast Cancer Invasive; Ovarian Carcinoma; Cervical Cancer; Non Small Cell Lung Cancer; Gastric Cancer; Biliary Tract Cancer; Melanoma; Pancreas Cancer; MDM2 Gene Amplification; Testicular Germ Cell Tumor; Adrenocortical Carcinoma	Rain Oncology Inc	2021-11-01	PHASE2
NCT04979442	TERMINATED	Dedifferentiated Liposarcoma	Rain Oncology Inc	2021-07-14	PHASE3
NCT05758818	TERMINATED	Cardiac Repolarization	Rain Oncology Inc	2023-04-17	PHASE1
NCT06090318	WITHDRAWN	Advanced Solid Tumor; CDKN2A; NSCLC; Urothelial Carcinoma Bladder; Melanoma; Pancreas Adenocarcinoma; HNSCC; Renal Cell Carcinoma; Mesothelioma; Gastric Cancer	Rain Oncology Inc	2023-05-19	PHASE1; PHASE2
NCT03634228	TERMINATED	Acute Myeloid Leukemia; Recurrent Acute Myeloid Leukemia; Refractory Acute Myeloid Leukemia	M.D. Anderson Cancer Center	2018-12-17	PHASE1; PHASE2

Tech Support

Handling Instructions

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